公开(公告)号：US20240336572A1

公开(公告)日：2024-10-10

申请号：US18626467

申请日：2024-04-04

Applicant: Pfizer Inc.

Inventor： Samit Kumar Bhattacharya ,  Edward Lee Conn ,  David Christopher Ebner ,  Brian Stephen Gerstenberger ,  Chan Woo Huh ,  Daniel Wei-Shung Kung ,  Alan Martin Mathiowetz ,  Jessica Gloria Katherine O'Brien ,  Meihua Mike Tu ,  Kimberly O'Keefe Cameron ,  Dilinie Prasadhini Fernando ,  Kevin James Filipski ,  Esther Cheng Yin Lee ,  Sarah Jane Mear ,  Aaron Christopher Smith

IPC: C07D231/56 ,  A61K31/416

CPC classification number: C07D231/56 ,  A61K31/416

Abstract: The invention relates to substituted indazole propionic acid derivatives, pharmaceutically acceptable salts, tautomers, or pharmaceutically acceptable salts of the tautomers thereof that can activate adenosine 5′-monophosphate-activated protein kinase (AMPK). The invention further relates to pharmaceutical compositions comprising AMPK-activating substituted indazole propionic acid derivatives, pharmaceutically acceptable salts, tautomers, or pharmaceutically acceptable salts of the tautomers thereof and at least one pharmaceutically acceptable excipient, and methods of treating a condition comprising administering AMPK-activating substituted indazole propionic acid derivatives, pharmaceutically acceptable salts, tautomers, or pharmaceutically acceptable salts of the tautomers thereof.

公开(公告)号：US20240109915A1

公开(公告)日：2024-04-04

申请号：US18359709

申请日：2023-07-26

Applicant: Pfizer Inc.

Inventor： Scott William Bagley ,  Andrea Nicole Bootsma ,  Chulho Choi ,  Robert Lee Dow ,  David James Edmonds ,  Carmen Noemi Garcia-Irizarry ,  Brian Stephen Gerstenberger ,  Gajendra Ingle ,  Jessica Gloria Katherine O'Brien ,  Mihir Dineshkumar Parikh ,  Gwenaella Christine Rescourio ,  Daniel Copley Schmitt

IPC: C07D513/10

CPC classification number: C07D513/10

Abstract: A compound having the structures:




or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate of said compound or pharmaceutically acceptable salt, wherein; R selected from the group consisting of H, C1-C6 alkyl, C1-C6 alkoxy and —(CH2)m—W, where W is C3-C8 cycloalkyl, bicycloalkyl, bridged bicycloalkyl, phenyl, 5- or 6-membered heteroaryl or heterocyclic containing one, two or three heteroatoms selected from the group consisting of N, S and O atoms; wherein each of said alkyl, cycloalkyl, alkoxy, heterocyclic, phenyl, naphthyl or heteroaryl may be unsubstituted or substituted by phenyl, halo, cyano, deuterium, hydroxy, C1-C6 alkyl, C1-C6 alkoxy, —SO2—R′, —CONR′R″, NR′COR″, —NR′CONR′R″, —NR′CO2R″, —(CH2)n—SO2—R′, —NHSO2—R′, —NR″SO2—R′, —SO2NR′R″, NR′R″ or SR′ where R′ and R″ are independently H, C1-C6 alkyl or C3-C8 cycloalkyl; R1 selected from the group consisting of phenyl, naphthyl, 5- or 6-membered heteroaryl or heterocyclic containing one, two, three or four heteroatoms selected from the group consisting of N, S and O atoms; and, a 9- or 10-membered bicyclic aryl, heteroaryl or heterocyclic containing one, two or three heteroatoms selected from the group consisting of N, S and O atoms; wherein each of said phenyl, naphthyl, aryl, heterocyclic, or heteroaryl may be unsubstituted or substituted by halo, cyano, deuterium, hydroxy, C1-C6 alkyl, C1-C6 alkoxy, phenyl, —SO2—R′, —CONR′R″, NR′COR″, —NR′CONR′R″, —NR′CO2R″, —(CH2)n—SO2—R′, —NHSO2—R′, —NR″SO2—R, —SO2NR′R″, —P(O)R′R″,




or NR′R″′ or SR′ where R′ and R″ are independently H, C1-C6 alkyl or C3-C8 cycloalkyl; and, m and n are independently 0, 1, 2 or 3. The invention also relates to pharmaceutically acceptable salts of these compounds and to pharmaceutically acceptable solvates thereof; to compositions containing such compounds; and to the uses of such compounds in the treatment of various diseases, particularly acne.